The present invention relates to a series of new azasteroid compounds which are useful for the treatment and prophylaxis of prostatic hypertrophy, and provides methods and compositions using them as well as processes for their preparation.
Available treatment for prostatic hypertrophy is very limited, although it has been shown that compounds which inhibit the activity of testosterone 5.alpha.-reductase may be useful for the treatment and prophylaxis of prostatic hypertrophy, and U.S. Pat. No. 4,179,453 and 4,760,071 disclose several compounds which have this type of activity and which may thus be useful for this purpose. Of these compounds, those which are the most active and are believed to be closest to the compounds of the present invention are the compounds of formula (A): ##STR2## in which R' and R" both represent ethyl groups (Compound A.sub.1), or R' represents a hydrogen atom and R" represents a t-butyl group (Compound A.sub.2). However, whilst these compounds do have quite a potent activity, there is a need to develop compounds having greater activity.
We have now discovered that compounds having certain specific carbamoyl substituents at the 17-position of the azasteroid skeleton have excellent 5.alpha.-reductase inhibitory activity, and can therefore be used for the type of treatment and prophylaxis referred to above.